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MedKoo Cat#: 127150 | Name: Lucitanib HCl
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Lucitanib is a dual inhibitor of VEGFR and FGFR that inhibits VEGFR1, VEGFR2, and VEGFR3 (IC50s = 7, 25, and 10 nM, respectively) and FGFR1 and FGFR2 (IC50s = 17.5 and 82.5 nM, respectively).

Chemical Structure

Lucitanib HCl
Lucitanib HCl
CAS#2108875-91-6 (HCl)

Theoretical Analysis

MedKoo Cat#: 127150

Name: Lucitanib HCl

CAS#: 2108875-91-6 (HCl)

Chemical Formula: C26H27Cl2N3O4

Exact Mass: 515.1379

Molecular Weight: 516.42

Elemental Analysis: C, 60.47; H, 5.27; Cl, 13.73; N, 8.14; O, 12.39

Price and Availability

Size Price Availability Quantity
1mg USD 250.00 2 Weeks
5mg USD 550.00 2 Weeks
10mg USD 850.00 2 Weeks
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Related CAS #
1058137-23-7 (free base) 2108875-91-6 (HCl)
Synonym
Lucitanib HCl; E3810; E-3810; E 3810; AL3810; AL 3810; AL-3810; Lucitanib
IUPAC/Chemical Name
6-((7-((1-aminocyclopropyl)methoxy)-6-methoxyquinolin-4-yl)oxy)-N-methyl-1-naphthamide dihydrochloride
InChi Key
GJYKJPXOPZOBBC-UHFFFAOYSA-N
InChi Code
InChI=1S/C26H25N3O4.2ClH/c1-28-25(30)19-5-3-4-16-12-17(6-7-18(16)19)33-22-8-11-29-21-14-24(23(31-2)13-20(21)22)32-15-26(27)9-10-26;;/h3-8,11-14H,9-10,15,27H2,1-2H3,(H,28,30);2*1H
SMILES Code
O=C(C1=CC=CC2=CC(OC3=CC=NC4=C3C=C(OC)C(OCC5(CC5)N)=C4)=CC=C21)NC.Cl.Cl
Appearance
To be determined
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 -4 C for short term (days to weeks) or -20 C for long term(months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 516.42 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Colzani M, Noberini R, Romanenghi M, Colella G, Pasi M, Fancelli D, Varasi M, Minucci S, Bonaldi T. Quantitative chemical proteomics identifies novel targets of the anti-cancer multi-kinase inhibitor E-3810. Mol Cell Proteomics. 2014 Jun;13(6):1495-509. doi: 10.1074/mcp.M113.034173. Epub 2014 Apr 2. PubMed PMID: 24696502; PubMed Central PMCID: PMC4047469. 2: Zangarini M, Ceriani L, Bello E, Damia G, Cereda R, Camboni MG, Zucchetti M. HPLC-MS/MS method for quantitative determination of the novel dual inhibitor of FGF and VEGF receptors E-3810 in tumor tissues from xenograft mice and human biopsies. J Mass Spectrom. 2014 Jan;49(1):19-26. doi: 10.1002/jms.3305. PubMed PMID: 24446259. 3: Bello E, Taraboletti G, Colella G, Zucchetti M, Forestieri D, Licandro SA, Berndt A, Richter P, D'Incalci M, Cavalletti E, Giavazzi R, Camboni G, Damia G. The tyrosine kinase inhibitor E-3810 combined with paclitaxel inhibits the growth of advanced-stage triple-negative breast cancer xenografts. Mol Cancer Ther. 2013 Feb;12(2):131-40. doi: 10.1158/1535-7163.MCT-12-0275-T. Epub 2012 Dec 27. PubMed PMID: 23270924. 4: Damia G, Colella G, Camboni G, D'Incalci M. Is PDGFR an important target for E-3810? J Cell Mol Med. 2012 Nov;16(11):2838-9. doi: 10.1111/j.1582-4934.2012.01601.x. PubMed PMID: 22805298. 5: Sala F, Bagnati R, Livi V, Cereda R, D'Incalci M, Zucchetti M. Development and validation of a high-performance liquid chromatography-tandem mass spectrometry method for the determination of the novel inhibitor of angiogenesis E-3810 in human plasma and its application in a clinical pharmacokinetic study. J Mass Spectrom. 2011 Oct;46(10):1039-45. doi: 10.1002/jms.1985. PubMed PMID: 22012670. 6: Bello E, Colella G, Scarlato V, Oliva P, Berndt A, Valbusa G, Serra SC, D'Incalci M, Cavalletti E, Giavazzi R, Damia G, Camboni G. E-3810 is a potent dual inhibitor of VEGFR and FGFR that exerts antitumor activity in multiple preclinical models. Cancer Res. 2011 Feb 15;71(4):1396-405. doi: 10.1158/0008-5472.CAN-10-2700. Epub 2011 Jan 6. PubMed PMID: 21212416. 7: Kawai T, Ikeda H, Harada Y, Saitou T. [Changes in the rat stomach after long-term administration of proton pump inhibitors (AG-1749 and E-3810)]. Nihon Rinsho. 1992 Jan;50(1):188-93. Japanese. PubMed PMID: 1311785